The estrogen metabolites 2-methoxyestradiol and 2-hydroxyestradiol inhibit endometriotic cell proliferation in estrogen-receptor-independent manner

Samartzis EP, Eleftherios Pierre Samartzis, Eleftherios P Samartzis, Patrick Imesch, Imesch P, Twiehaus A, Anja Twiehaus, Raghvendra K. Dubey, Brigitte Leeners
Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology · 2016 · vol. 32(7) , pp. 529–533 · doi:10.3109/09513590.2015.1137094 · PMID:26800447 · W2290229020
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Estrogen metabolites 2-methoxyestradiol and 2-hydroxyestradiol inhibited endometriotic cell proliferation in pharmacological doses through partially estrogen-receptor-independent mechanisms.

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Abstract

Endometriosis, a painful disorder associated with infertility, is estimated to occur in approximately 7-10% of reproductive age women. Although endometriosis is considered as an estrogen-dependent disease, the role of estrogen metabolites via receptor-independent mechanisms has not yet been comprehensively clarified. In the present study, growth studies were performed comparing the effect of estradiol (E2), estrogen metabolites, that is, 2-hydroxyestradiol (2-OHE2) and 2-methoxyestradiol (2-ME), as well as estrogen-receptor-independent mechanisms using the estrogen receptor antagonist fulvestrant, on cell proliferation of endometriotic cells. The estrogen metabolites 2-OHE2 and 2-ME inhibited cell growth in a dose-dependent manner in pharmacological doses. Lower concentrations of 2-OHE2 had a stimulating effect on cell proliferation while pharmacologic doses exerted an antimitogenic effect. The effects on cell growth were at least partially receptor-independent, as demonstrated by simultaneous receptor antagonization with fulvestrant. In conclusion, our results demonstrate that in pharmacological doses the estrogen metabolites 2-ME and 2-OHE2 show inhibiting effects on the proliferation of endometriotic cells and may be promising substances for the treatment of endometriosis.

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Condition tags

endometriosisinfertility

MeSH descriptors

Cell Proliferation Endometriosis Estradiol Estrogen Receptor Antagonists 2-Methoxyestradiol 2-Methoxyestradiol Cell Line Cell Line Cell Proliferation Cell Proliferation Dose-Response Relationship, Drug Dose-Response Relationship, Drug Endometriosis Endometriosis Estradiol Estradiol Estradiol Estrogen Receptor Antagonists Estrogen Receptor Antagonists Female

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